Co-trimoxazole-acres
Active material: Co-trimoxazole [Sulfamethoxazole + Trimethoprim]
When ATH: J01EE01
CCF: Antibacterial drug sulfanilamide
ICD-10 codes (testimony): A01, A02, A03, A04.0, A09, A23, A38, A54, A55, A57, B40, B50, B51, B52, B58, B59, H66, J01, J02, J03, J04, J15, J20, J31, J32, J35.0, J37, J42, J47, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, L70, M86, N10, N11, N30, N34, N41, N45, T79.3
When CSF: 06.16.01
Manufacturer: Chemical-Pharmaceutical Plant JSC QUINACRINE (Russia)
Pharmaceutical form, composition and packaging
Pills white or white with Valium a color shade, Valium, chamfered.
| 1 tab. | |
| sulfamethoxazole | 400 mg |
| trimethoprim | 80 mg |
Excipients: potato starch, magnesium stearate, polyvinylpyrrolidone.
20 PC. – packings Valium planimetric.
Pharmacological action
Combined antimicrobial, consisting of sulfamethoxazole and trimethoprim. Sulfamethoxazole, similar in structure to para-aminobenzoic acid (PABA), It gives dihydrofolic acid synthesis in bacterial cells, preventing the inclusion of PABA in its molecule. Trimethoprim-sulfamethoxazole enhances the action, violating recovery digidrofolievoy tetrahydrofolic acid – the active form of folic acid, responsible for protein metabolism and microbial cell division.
It is a bactericidal broad-spectrum drugs, active against the following microorganisms: Streptococcus spp. (hemolytic strains are more sensitive to penicillin), Staphylococcus spp., Streptococcus pneumoniae, Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including strains enterotoksogennye), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi), Vibrio cholerae, Bacillus anthracis, Haemophilus influenzae (including ampicillin resistance strains), Listeria spp., Nocardia asteroids, Bordetella pertussis, Enterococcus faecalis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Mycobacterium spp. (incl. Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumophila, Providence, some species Pseudomonas (other than Pseudomonas aeruginosa), Serratia wilting, Shigella spp., Yersinia spp., Morganella spp., Pneumocystis carinii; Chlamydia spp. (incl. Chlamydia trachomatis, Chlamydia psittaci); protozoa: Plasmodium spp., Toxoplasma gondii, pathogenic fungi, Actinomyces israelii, Merciless coccidioides, Histoplasma capsulatum, Leishmania spp.
Drug resistance: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., viruses.
Inhibits E. coli livelihoods, which leads to reduced synthesis of thymine, riʙoflavina, nicotinic acid, etc.. B vitamins in the intestine.
Pharmacokinetics
In peroralynom accept absorption – 90%. TCmax – 1-4 no, therapeutic concentration level is maintained 7 h after a single dose. It is well distributed in the body. It penetrates through the BBB, the placenta and breast milk. The lungs and urine concentrations creates, excess plasma levels. To a lesser extent in the bronchial secretions accumulate, vaginal secretions, secretions and tissues of the prostate, middle ear fluid (when inflammation), cerebrospinal fluid, bile, bones, saliva, the aqueous humor of the eye, breast milk, interstitial fluid. Relationship to plasma proteins – 66% in sulfamethoxazole, trimethoprim in – 45%.
Mostly sulfamethoxazole is metabolised to produce acetylated derivatives. Metabolites possess an antimicrobial activity.
Excreted by the kidneys as metabolites (80% during 72 no) and unaltered (20% sulfamethoxazole, 50% Trimethoprim); negligible quantity – through the intestine. T1/2 sulfamethoxazole – 9-11 no, Trimethoprim – 10-12 no, children – significantly less, depending on the age: to 1 year – 7-8 no, 1-10 years – 5-6 no. In elderly and patients with impaired renal function T1/2 increases.
Testimony
- Infections of urinary organs: uretrit, cystitis, pyelitis, pyelonephritis, prostatitis, epididymitis, gonorrhea (male and female), chancroid, lymphogranuloma venereum, inguinal pellets;
- Respiratory tract infections: bronchitis (acute and chronic), bronchiectasis, lobar pneumonia, bronchopneumonia, Pneumonia;
- Infections of upper respiratory tract: otitis media, sinusitis, laringit, sore throat; scarlet fever;
- Infections of the digestive tract: typhoid fever, paratif, salmonellonositelstvo, cholera, dysentery, cholecystitis, kholangit, gastroenteritis, вызванные энтеротоксичными штаммами Escherichia coli;
- Infections of the skin and soft tissues: acne, furunculosis, pyoderma, wound infections;
- Osteomyelitis (acute and chronic) and etc. osteoartikulyarnye infection, Brucellosis (sharp), South American blastomycosis, malaria (Plasmodium falciparum), toxoplasmosis (in the complex therapy).
Dosage regimen
Inside, I /, / m. In each dosage form, the quantitative ratio of trimethoprim and sulfamethoxazole 1:5.
Inside (tablets), adults and children over 12 years – 960 mg dose, or 480 mg 2 once a day. In severe During infections – by 480 mg 3 once a day, at chronic infections maintenance dose – 480 mg 2 once a day. Children 1-2 years – 120 mg 2 once a day, 2-6 years – 120-240 mg 2 once a day, 6-12 years – 240-480 mg 2 once a day.
Suspension: children 3-6 Months – 120 mg 2 once a day, 7 months-3 years – 120-240 mg 2 once a day, 4-6 years – 240-480 mg 2 once a day, 7-12 years – 480 mg 2 once a day, adults and children over 12 years – 960 mg 2 once a day. Syrup for children: children 1-2 years – 120 mg 2 once a day, 2-6 years – 180-240 mg 2 once a day, 6-12 years – 240-480 mg 2 once a day.
The minimum duration of treatment – 4 day; Once the symptoms continue therapy for 2 days. In chronic infections treatment longer. At Acute brucellosis – 3-4 Sun, at typhoid and paratyphoid – 1-3 Months.
To prevention of relapse of chronic urinary tract infections adults and children over 12 years – 480 mg 1 once a day at night, Children up to 12 years – 12 mg / kg / day. Duration of treatment – 3-12 Months. The treatment of acute cystitis in children 7-16 years – 480 mg 2 twice a day for 3 days.
At gonorrhea – 1920-2880 mg / day for 3 admission.
At gonorejnom faringite (hypersensitivity to penicillin) – 4320 mg 1 once a day for 5 days. At pneumonia, caused by Pneumocystis carinii, – 120 mg / kg / day intervals 6 h for 14 days.
Parenteral: / m adults and children over 12 years – 480 mg every 12 no, children 6-12 years – 240 mg every 12 no.
B / drip, adults and children over 12 years – 960-1920 mg every 12 no, children 6-12 years – 480 mg 2 once a day; 6 months-5 years – 240 mg 2 once a day; 6 Sun, 5 months – 120 mg 2 once a day.
For maximum efficiency, a constant concentration of trimethoprim in plasma or serum should be maintained at 5 ug / ml or higher.
Malaria, вызываемая Plasmodium falciparum, – in / Infusion (1920 mg 2 once a day) during 2 days. Babies need a lower dose, respectively.
To achieve higher concentrations in the CSF is administered in / in the drip (rastvoriv 200 mL of solvent) during 1 no 2 once a day.
At renal failure dose depends on the value QC: at QC over 25 ml / min – the standard dose; at 15-25 ml / min – The standard dose for 3 days, then half the standard dose. At CC less than 15 ml / mYing appoint half the standard dose only against the background of hemodialysis.
Dissolving in the following proportions immediately before administration: 480 mg (5 ml solution for infusion) on 125 ml, 960 mg (10 ml) – on 250 ml, 1440 mg (15 ml) – on 500 ml infusion solution.
When the turbidity or crystallization solution before or during infusion of the mixture can not be used. Duration of administration – 1-1.5 no (It should be consistent with the needs of the patient in liquid).
If necessary to limit the amount of fluid injected is administered in higher concentrations – 5 ml dissolved in 50-75 ml 5% dextrose in water. In severe infections in all age groups, the dose may be increased by 50%.
Side effect
From the nervous system: headache, dizziness; in some cases – aseptic meningitis, depression, apathy, tremor, peripheral neuritis.
The respiratory system: bronchospasm, pulmonary infiltrates.
From the digestive system: nausea, vomiting, decreased appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, activity increase “Hepatic” transaminases, hepatitis, gepatonekroz, pseudomembranous enterocolitis.
From the side of hematopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastnaya anemia.
From the urinary system: polyuria, interstitial nephritis, impairment of renal function, kristallurija, hematuria, increasing concentrations of urea, giperkreatininemiя, toksicheskaya nephropathy oliguriey and anuriey.
On the part of the musculoskeletal system: arthralgia, myalgia.
Allergic reactions: itch, photosensitivity, rash, erythema multiforme exudative (incl. Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioedema, redness of the sclera.
Local reactions: tromboflebit (in the site of the venipuncture), tenderness at the injection site.
Other: gipoglikemiâ.
Contraindications
- Hypersensitivity (incl. to sulfonamides);
- Liver failure;
- Renal failure (CC less than 15 ml / min);
- Aplasticheskaya anemia;
— B12-defitsitnaya anemia;
- Agranulocytosis, leukopenia;
- Deficiency of glucose-6-fosfatdegidrogenazы;
- Pregnancy;
- Lactation;
- Up to 6 years (for the / m);
- Children's age (to 3 Months – orally);
- Hyperbilirubinemia in children.
FROM caution: folic acid deficiency, bronchial asthma, thyroid disease.
Pregnancy and lactation
Is contraindicated in pregnancy and lactation.
Cautions
It is advisable to determine the concentration of sulfamethoxazole in plasma every 2-3 days immediately before the next infusion. If the concentration exceeds sulfamethoxazole 150 ug / ml, treatment should be interrupted until, until it drops below 120 ug / ml.
At long (more than a month) courses of treatment requires regular blood tests, because there is the risk of hematological changes (often asymptomatic). These changes may be reversible when assigning folic acid (3-6 mg / day), that does not significantly impair the antimicrobial activity of the drug. Particular caution should be shown in the treatment of elderly patients or patients with suspected initial lack of folate. Purpose of folic acid is also advisable when chronic treatment with high doses.
To prevent crystalluria is recommended to maintain a sufficient volume of urine. Chance of toxic and allergic complications of sulfonamides substantially increases with a decrease in kidney filtration function.
It is inappropriate and against the background of the treatment consumed foods, contain large quantities of PABA, – green parts of plants (cauliflower, spinach, pulse), carrot, tomatoes.
Avoid excessive sun and UV radiation.
The risk of side effects is significantly higher in patients with AIDS.
Not recommended for tonsillitis and pharyngitis, caused by beta-hemolytic streptococcus group A, because of widespread resistance strains.
Overdose
Symptoms: nausea, vomiting, kišečnaâ how, dizziness, headache, drowsiness, depression, fainting, confusion, blurred vision, fever, hematuria, kristallurija; For prolonged overdose – thrombocytopenia, leukopenia, megaloblastnaya anemia, jaundice.
Treatment: gastric lavage, Acidification of urine increases the excretion of trimethoprim, fluid intake by mouth, / m – 5-15 mg / day calcium folinate (It eliminates the effects of trimethoprim on the bone marrow), if necessary – hemodialysis.
Drug Interactions
The pharmaceutically compatible with the following drugs: Dextrose for in / infusion 5 and 10%, levulose for in / infusion 5%, Sodium chloride for in / infusion 0.9%, mixture 0.18% sodium and hloridal 4% dextrose for in / infusion, 6% dextran 70 for / in infusion 5% or dextrose 0.9% sodium chloride solution, 10% dextran 40 for / in infusion 5% or dextrose 0.9% sodium chloride solution, Ringer solution for injections.
It increases the anticoagulant activity of indirect anticoagulants, and the action of hypoglycemic drugs and methotrexate.
It reduces the intensity of the hepatic metabolism of phenytoin (extends its T1/2 on 39%) and warfarin, increasing their effect.
Reduces the reliability of oral contraceptives (It inhibits the intestinal microflora and reduce enterohepatic circulation hormonal compounds).
Rifampicin reduces T1/2 Trimethoprim.
Pyrimethamine doses, exceeding 25 mg / Sun, It increases the risk of megaloblastic anemia.
Diuretic (often thiazides) increase the risk of thrombocytopenia.
Reduces the effect of benzocaine, prokayn, prokaynamyd (and other drugs, by hydrolysis which is formed PABA).
Between diuretics (tiazidы, furosemide et al.) and oral hypoglycemic drugs sredsvami (sulfonylureas), one side, and antimicrobial sulfonamides – with another, possible development of cross-allergic reaction.
Phenytoin, barbiturates, PAS increase the expression of folate deficiency.
Salicylic acid derivatives enhance the effect of.
Cholestyramine reduces the absorption of, it should be taken over 1 h after or 4-6 hours prior to receiving co-trimoxazole.
PM, suppress bone marrow hemopoiesis, increase the risk of myelosuppression.
